AChR

Forskolin (Coleonol) is a natural product, an adenylate cyclase activator (EC50=0.5 μみゅーM). Forskolin increases cAMP levels, activates PXR and FXR, and induces autophagy. Forskolin produces positive inotropic effects in the heart, and has platelet anticoagulant and antihypertensive effects.

(R,S)-Anatabine is a minor tobacco alkaloid found in the Solanaceae family of plants, and serves as a specific marker for detecting tobacco use.

Pilocarpine Hydrochloride (NSC 5746 HCl) , a nonselective muscarinic acetylcholine receptor agonist, is utilized to produce an experimental model of epilepsy.

Procainamide Hydrochloride (Procapan) is the hydrochloride salt form of procainamide, an amide derivative exhibiting class 1A antiarrhythmic property and analog of procaine. Procainamide hydrochloride reversibly binds to and blocks activated (open) voltage-gated sodium channels, thereby blocks the influx of sodium ions into the cell, which leads to an increase in threshold for excitation and inhibit depolarization during phase 0 of the action potential.

Cytisinicline (Sophorine), an alkaloid, is found naturally in several plants.

Solifenacin succinate (YM905) is a quinuclidine and tetrahydroisoquinoline derivative and selective M3 MUSCARINIC ANTAGONIST. It is used as a UROLOGIC AGENT in the treatment of URINARY INCONTINENCE.

Methscopolamine (Hyoscine methyl bromide) (Pamine), as a natural plant alkaloid, is a muscarinic acetylcholine receptor blocker.

Olanzapine (LY170053) is an atypical antipsychotic that is used currently in the treatment of schizophrenia and bipolar illness.

Bambuterol hydrochloride (KWD-2183 hydrochloride) , a long-acting beta-adrenoceptor agonist, is utilized for the treating of asthma.

Atracurium besylate (51W89) is a non-depolarizing neuromuscular blocking agent with short duration of action. Its lack of significant cardiovascular effects and its lack of dependence on good kidney function for elimination provide clinical advantage over alternate non-depolarizing neuromuscular blocking agents.

Nicardipine hydrochloride (YC-93 Hydrochloride) is the hydrochloride salt form of nicardipine, a synthetic derivative of nitrophenyl-pyridine and potent calcium channel blocker, Nicardipine (Nifedipine Family) blocks calcium ions from certain cell walls and inhibits contraction of coronary and peripheral arteries, resulting in lowered oxygen requirements for heart muscle and decreased arterial contraction and spasm. It is used clinically as a cerebral and coronary vasodilator.

Bethanechol chloride (Carbamyl-βべーた-methylcholine chloride) is a slowly hydrolyzing muscarinic agonist with no nicotinic effects. It is used to increase smooth muscle tone in the GI tract following abdominal surgery or to treat urinary retention without obstruction. Possible side effects include hypotension, heart rate changes, and bronchial spasm.

Scopoletin (Esculetin 6-methyl ether) is a plant growth factor derived from the root of Scopolia carniolica, inhibits of acetylcholinesterase (AChE).

4-Hydroxycoumarin is a coumarin derivative and one of the versatile heterocyclic scaffolds with electrophilic and nucleophilic properties.

Metoclopramide hydrochloride (Metoclopramide HCl) is a selective dopamine D2 receptor antagonist, used as an antiemetic.

Fipexide (Attentil, Vigilor), a psychoactive drug of the piperazine chemical class, was developed in Italy in 1983. It was served as a nootropic drug in France and Italy, mainly for the therapy of senile dementia, but is no longer in common use because of the occurrence of rare drug side-effects including hepatitis and fever.

Neostigmine methyl sulfate (Syntostigmin) is a reversible inhibitor of acetylcholinesterase, can not cross the blood-brain barrier, used in the treatment of myasthenia gravis.

Propoxur (Propoxure) is an insecticide used to control cockroaches, flies, mosquitoes, and lawn and turf insects. Acute (short-term) exposure of humans to propoxur by ingestion leads to cholinesterase inhibition of red blood cells, with mild cholinergic symptoms including blurred vision, nausea, vomiting, sweating, and tachycardia; however, the effects are transient. Chronic (long-term) inhalation exposure has resulted in depressed cholinesterase levels, headaches, vomiting, and nausea in humans. Chronic ingestion studies in animals have reported depressed cholinesterase levels, depressed body weight, effects to the liver and bladder, and a slight increase in neuropathy. No information is available on the reproductive, developmental, or carcinogenic effects of propoxur in humans. Mixed results are available from cancer studies of propoxur in animals. EPA has not classified propoxur for carcinogenicity.

Tolterodine tartrate (PNU-200583E) is a potent antagonist for muscarinic receptor. It show selectivity for the urinary bladder and salivary glands in vivo.

Solifenacin (YM905 free base) (YM905 free base) is a novel muscarinic receptor antagonist, its pKis for M1, M2 and M3 receptors is of 7.6, 6.9 and 8.0, respectively.

Clothianidin (TI 435), an insecticide, acts as an agonist of acetylcholine to stimulate nAChR, thereby activating post-synaptic acetylcholine receptors but not inhibiting AChE.

Hexamethonium Bromide (Hexamethonium Dibromide), a specific antagonist of neuronal-type nicotinic AChR in ganglia, is poorly absorbed from the gastrointestinal tract and does not cross the blood-brain barrier.

Mitotane (NCI-C04933) is a derivative of the insecticide DICHLORODIPHENYLDICHLOROETHANE that specifically inhibits cells of the adrenal cortex and their production of hormones. It is used to treat adrenocortical tumors and causes CNS damage, but no bone marrow depression.

Diphenmanil methylsulfate (Diphemanil mesylate), a quaternary ammonium anticholinergic, binds muscarinic acetylcholine receptors and thus decreases secretory excretion of stomach acids, sweat, and saliva.

Carbachol (Carbamoylcholine chloride), an analog of acetylcholine, serves as a valuable tool in the investigation of various physiological responses mediated by nicotinic (nAChR) and muscarinic (mAChR) acetylcholine receptors. These responses include smooth muscle contraction, gut motility, and neuronal signaling. Known for its agonistic properties, Carbachol activates both nAChR and mAChR, with reported Ki values ranging from 10 to 10,000 nM for different receptor types and experimental preparations.

Anethole trithione (Anetholtrithion) is a bile secretion-stimulating drug that restores salivation and relieves the discomfort of dry mouth in chemotherapy-induced xerostomia.

Vecuronium bromide (ORG NC 45) is a synthetic, intermediate-acting, mono-quaternary steroid that functions as a non-depolarizing neuromuscular blocking agent with muscle relaxant properties.

Carbetapentane citrate (Pentoxyverine citrate) , an antitussive (cough suppressant), is frequently used for a cough related to illnesses like the common cold.

1. Palmatine (Burasaine) is an inhibitor of dopamine generation. 2. Palmatine could potentially be developed for the treatment of flavivirus infections. 3. Palmatine has been used in the treatment of jaundice, dysentery, hypertension, inflammation, and liver-related diseases.

Racanisodamine (7βべーた-Hydroxyhyoscyamine) is an anticholinergic and αあるふぁ1-adrenergic receptor antagonist used in the treatment of acute circulatory shock.

Benzethonium chloride (Quatrachlor) is a synthetic quaternary ammonium salt with surfactant, antiseptic, and broad spectrum antimicrobial properties.

Methylbenactyzium Bromide (Semulgin) is an anticonvulsant that is the active metabolite of trimethadione.

Molindone hydrochloride (EN-1733A) is an indole derivative effective in treating schizophrenia and other psychoses by blocking dopamine's effects in the brain.

Coluracetam (MKC-231)(MKC-231) is a Choline Uptake Enhancer.

Dibucaine (Cinchocaine), a local anesthetic of the amide type, is now usually used for surface anesthesia.

Ribavirin (Tribavirin) is a synthetic nucleoside analog of ribofuranose with activity against hepatitis C virus and other RNA viruses.

Aniracetam (Ro 13-5057)(Ro 13-5057), a nootropic and neuroprotective drug, selectively modulates the AMPA receptor and nAChR.

Galanthamine hydrobromide (Galantamine hydrobromide), a long-acting and centrally active AChE inhibitor (IC50:410 nM), is an allosteric potentiator at neuronal nicotinic ACh receptors.

(+)-Sparteine (Pachycarpine) is a natural product extracted from scotch broom, is a sodium channel blocker and a class 1a antiarrhythmic agent

Dinotefuran (MTI-446) is an insecticide of the neonicotinoid class for control of insect pests such as aphids, whiteflies, thrips, leafhoppers, leafminers. Its mechanism of action involves disruption of the insect's nervous system by inhibiting nicotinic acetylcholine receptors.

Darifenacin hydrobromide (UK-88525) is a selective muscarinic receptor antagonist used to treat urinary incontinence and overactive bladder syndrome.

Decamethonium bromide (Syncurine) is a neuromuscular blocker and nicotinic AChR partial agonist.

Propantheline bromide (Pro-Banthine) competitively antagonizes acetylcholine activity mediated by muscarinic receptors at neuroeffector sites on smooth muscle and exocrine gland cells. Propantheline Bromide is the bromide salt form of propantheline, a quaternary ammonium compound structurally related to belladonna alkaloids. An aspartic acid residue present in the N-terminal portion of the third transmembrane helix of the muscarinic receptor is believed to form an ionic bond with the tertiary or quaternary nitrogen of the antagonist. Antagonism leads to a reduction of exocrine glands secretions and to relax the bronchial muscle and reduce tone and motility of intestinal smooth muscle.

Mebhydrolin napadisylate (Incidal) is an antihistamine used to relieve allergic symptoms caused by histamine release, including nasal allergies and allergic dermatosis.

Choline bitartrate (2-hydroxyethyl(trimethyl)azanium) is a form of the nutrient choline which is found in foods. Choline is necessary for normal liver and kidney function and a component of the neurotransmitter acetylcholine, a chemical that facilitates communication between the nerves and muscles.